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Pharmacology for FRCR CO1 > 2.6 Clinical pharmacology of analgesics > Flashcards

2.6 Clinical pharmacology of analgesics Flashcards

1
Q

What is the bioavailability of morphine?

A

Oral - 35%

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2
Q

How quick is the onset of action for sc Morphine?

A

10-20 min

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3
Q

What is the halflife of morphine - PO and IV?

A

PO 2-3h
IV 1.5h

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4
Q

What is the duration of morphine immediate and modified release?

A

2-3 hours IR
12-24 hours MR

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5
Q

How is morphine metabolised?

A

First pass
UGT2B7

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6
Q

What are the metabolites of morphine?

A

M6G active
M3G inactive

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7
Q

What areceptor does morphine act on?

A

u - opioid

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8
Q

How quick is the onset for sc diamorphine?

A

5-10 min

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9
Q

What is the half life if IV diamorphine?

A

3 minutes

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10
Q

What is the duration of action of diamoprhine?

A

4 hours

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11
Q

What are the metabolites of diamorphine?

A

6-MAM
M6G
M3G

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12
Q

What receptor does diamorpgine act on

A

delta, mu, K

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13
Q

What is the bioavailability of oral oxycodone?

A

75% PO

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14
Q

How quick is the onset of action of oxycodone?

A

20-30 minutes

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15
Q

What is the halflife of oxycodone?

A

3.5 hours

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16
Q

What is the duration of action of oxycodone?

A

4-6 hours IR
12 hours MR

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17
Q

How is oxycodone metabolised?

A

CYP2D6
CYP3A4

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18
Q

What are the metabolites of oxycodone?

A

Oxymorphone
Noroxycodone

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19
Q

What receptors does oxycodone act on?

A

mu and K

20
Q

How quick is the onset of action of fentanyl?

A

3-23 hours

21
Q

What is the half life of fentanyl?

A

13-22 hours

22
Q

What is the duration of action of fentanyl?

A

72 hours with a patch
1-3.5 hours with lollipop

23
Q

How is fentanyl metabolised?

A

CYP3A4
CYP3A5

24
Q

What are the metabolites of fentanyl?

A

Norfentanyl

25
Q

What receptors does fentanyl act on?

A

u opioid

26
Q

How quick does Buprenorphine act?

A

18-24 hours

27
Q

What is the duration of action of buprenorphine?

A

7 days

28
Q

How is buprenorphine metabolysed?

A

CYP3A4

29
Q

How quickly does Alfentanyl act?

A

<1 min IV
<5 min IM

30
Q

What is the halflife of alfentanyl?

A

30 min IV
60 min IM

31
Q

How is alfentanyl metabolised?

A

CYP3A4 to inactivate metabolites secreted in urine

32
Q

What is level 1 of the analgesic ladder?

A

Paracetamol
- acts centrally and peripherally
- antipyretic

33
Q

What is level 2 of the analgesic ladder?

A

Weak opioids e.g. codeine, tramadol and dihydrocodenie

Tramadol 150mg = codeine 60mg

Also has some smooth muscle effetcs - causes constipation, suppresses cough

34
Q

What does tramadol act on?

A

Noradrenaline and 5HT uptake in spinal cord

35
Q

What are the optiond for level 3 analgesia?

A
  • Morphine
  • Toxicity
  • Fentanyl
  • Dextromoradine
36
Q

What toxicities are associated with opioids?

A

Drowsiness
Constipation
Nausea/vomiting
Dry mouth
Vivid dreams/hallucinations

37
Q

Why might pain not respond to opioids?

A
  • Opioid irrelevant e.g. neuropathic
  • Opioid tolerance
  • Opioid resistant
38
Q

How do you switch from oral immediate release morphine or oxycodone to a patch?

A

Apply patch, continue 4 hourly oral for 12 hours

39
Q

How do you switch from MR morphine or oxycodone to a patch?

A

Apply patch at same time as 12 hourly dose then stop

40
Q

How do you switch from driver of morphine, diamorphine, oxycodone, fentanyl?

A

Apply the patch and continue pump for 12 hours

41
Q

What are the step 1 adjuncts?

A

NSAIDs e.g. celecoxib

Steroids

42
Q

What are the step 2 adjuncts?

A

TCA e.g. amitryptiline
or
Antieplipetic e.g. gaba, pregab,

43
Q

What are the step 3 adjuncts?

A

TCA and antiepileptic

44
Q

What are the step 4 adjuncts?

A

NMDA receptor channel blocker e.g ketamine

45
Q

What are the step 5 adjuncts?

A

Spinal blocks

46
Q

What other adjuncts could be used?

A

Muscle relaxant e.g. baclofen, dantrolene, benzos

Bisphosphonates e.g. xometa

Supportive e.g. TENs, acupuncture

Pharmacology for FRCR CO1 (7 decks)

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